Tamoxifen citrate-ginsenoside co-amorphous substance as well as preparation method and pharmaceutical composition thereof

A technology of tamoxifen and ginsenoside, which is applied in the field of medicine, can solve the problems of low solubility and dissolution rate, and achieve the effect of increasing solubility and dissolution rate, and improving physical stability

Active Publication Date: 2020-11-13
NEOFORM BIOPHARMACEUTICAL LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0022] The technical problem to be solved by the present invention is to provide a tamoxifen citrate-ginsenoside co-amorphous substance and a preparation method thereof for the above-mentioned defects of low solubility and dissolution rate of the prior art, and Shaped pharmaceutical composition

Method used

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  • Tamoxifen citrate-ginsenoside co-amorphous substance as well as preparation method and pharmaceutical composition thereof
  • Tamoxifen citrate-ginsenoside co-amorphous substance as well as preparation method and pharmaceutical composition thereof
  • Tamoxifen citrate-ginsenoside co-amorphous substance as well as preparation method and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Embodiment 1, preparation of co-amorphous substance of tamoxifen citrate-ginsenoside

[0065] Weigh tamoxifen citrate and ginsenoside at a mass ratio of 1:2, and add a mixed solvent of methanol and dichloromethane (1:2 volume ratio) to form a solution. Transfer the solution to a volumetric flask, and add a certain volume of solvent to make up to volume.

[0066] The co-amorphous form of tamoxifen citrate-ginsenoside obtained was passed through a Büchi miniature spray dryer B290 equipped with an inert cycle B295 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 1.

[0067] Table 1

[0068] parameter Settings Suction 40kg / h Inlet temperature 100℃ output temperature 65℃ Injection rate 8mL / min ...

Embodiment 2

[0070] Embodiment 2, preparation of co-amorphous substance of tamoxifen citrate-ginsenoside

[0071] Weigh tamoxifen citrate and ginsenoside at a mass ratio of 1:2, and add a mixed solvent of methanol and dichloromethane (1:1 volume ratio) to form a solution. Transfer the solution to a volumetric flask, and add a certain volume of solvent to make up to volume.

[0072] The co-amorphous form of tamoxifen citrate-ginsenoside obtained was passed through a Büchi miniature spray dryer B290 equipped with an inert cycle B295 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 2.

[0073] Table 2

[0074] parameter Settings Suction 40kg / h Inlet temperature 95℃ output temperature 63℃ Injection rate 8mL / min ...

Embodiment 3

[0076] Embodiment 3, preparation of co-amorphous substance of tamoxifen citrate-ginsenoside

[0077] Weigh tamoxifen citrate and ginsenoside at a mass ratio of 1:2, and add a mixed solvent of methanol and dichloromethane (1:3 volume ratio) to form a solution. Transfer the solution to a volumetric flask, and add a certain volume of solvent to make up to volume.

[0078] The co-amorphous form of tamoxifen citrate-ginsenoside obtained was passed through a Büchi miniature spray dryer B290 equipped with an inert cycle B295 ( Labortechnik AG, Switzerland) spray-dried separation. A high-performance cyclone separator is used for separation, and the 50mL blue cap flask can be directly mounted to the cyclone separator for product collection. The parameter settings of the spray drying process are shown in Table 3.

[0079] table 3

[0080]

[0081]

[0082] After spray drying, the product was dried in an oven at 50°C under reduced pressure to remove excess solvent, and then XR...

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Abstract

The invention relates to a tamoxifen citrate-ginsenoside co-amorphous substance as well as a preparation method and a pharmaceutical composition thereof. According to the tamoxifen citrate-ginsenosideco-amorphous substance, Cu-Kalpha radiation is used, and an X-ray powder diffraction pattern expressed by 2theta has no sharp diffraction peak. After tamoxifen citrate and ginsenoside form the co-amorphous substance, the physical stability of the tamoxifen citrate-ginsenoside co-amorphous substance is remarkably improved compared with that of an amorphous physical mixture, the feasibility of thepatent medicine is achieved, and meanwhile, the solubility and the dissolution rate of tamoxifen citrate and the ginsenoside are remarkably improved compared with those of crude drugs.

Description

technical field [0001] The invention relates to the technical field of medicine, and more specifically, relates to a tamoxifen citrate-ginsenoside co-amorphous substance, a preparation method thereof, and a pharmaceutical composition containing the amorphous substance. Background technique [0002] Breast cancer is the most common malignant tumor in women. The global incidence of breast cancer has been on the rise since the late 1970s. Breast cancer has become a major public health problem in the current society. [0003] Current clinical treatment options for breast cancer include surgery, radiotherapy, chemotherapy, endocrine therapy, biological targeted therapy, and adjuvant therapy with traditional Chinese medicine. [0004] In recent years, endocrine therapy has gradually become a hot spot. Endocrine therapy aims to inhibit the growth of tumor cells by reducing the level of estrogen in the body or inhibiting the effect of estrogen. [0005] Studies have shown that most...

Claims

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Application Information

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IPC IPC(8): C07C217/14C07C213/10C07C59/265C07C51/43C07J17/00A61K31/704A61K31/138A61P35/00
CPCC07C217/14C07C59/265C07J17/005A61P35/00C07B2200/13
Inventor 田芳高明宋小叶
Owner NEOFORM BIOPHARMACEUTICAL LTD
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